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Assay Detail

CHEMBL2399239

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Binding
Binding affinity to human GST-tagged Bcl-Xl by luminescence proximity assay
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bcl-2-like protein 1 (CHEMBL4625) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G.
J Med Chem (2013) 56 : 5514 -5540
PubMed 23767404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.30 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376408 ABT 737 1.0 1 9.30
CHEMBL2398255 — — 1 8.22
CHEMBL2398250 — — 1 8.00
CHEMBL2398254 — — 1 7.85
CHEMBL2398252 — — 1 7.77
CHEMBL2398173 — — 1 7.64
CHEMBL2398260 — — 1 7.62
CHEMBL2398257 — — 1 7.33
CHEMBL2398249 — — 1 7.31
CHEMBL2398258 — — 1 7.29
CHEMBL2398253 — — 1 7.26
CHEMBL2398261 — — 1 7.22
CHEMBL2398263 — — 1 7.22
CHEMBL2398259 — — 1 7.11
CHEMBL2398256 — — 1 7.00
CHEMBL2398286 — — 1 6.92
CHEMBL2398172 — — 1 6.89
CHEMBL2398289 — — 1 6.82
CHEMBL2398251 — — 1 6.58
CHEMBL2398262 — — 1 6.47
CHEMBL2398283 — — 1 5.96
CHEMBL2398170 — — 1 5.92
CHEMBL2398285 — — 1 5.89
CHEMBL2398265 — — 1 5.82
CHEMBL2398284 — — 1 5.82
CHEMBL2398282 — — 1 5.80
CHEMBL2398296 — — 1 5.77
CHEMBL2398171 — — 1 5.77
CHEMBL2398266 — — 1 5.75
CHEMBL2398264 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376408 ABT 737 IC50 = 0.5 nM 9.30
CHEMBL2398255 — IC50 = 6.0 nM 8.22
CHEMBL2398250 — IC50 = 10.0 nM 8.00
CHEMBL2398254 — IC50 = 14.0 nM 7.85
CHEMBL2398252 — IC50 = 17.0 nM 7.77
CHEMBL2398173 — IC50 = 23.0 nM 7.64
CHEMBL2398260 — IC50 = 24.0 nM 7.62
CHEMBL2398257 — IC50 = 47.0 nM 7.33
CHEMBL2398249 — IC50 = 49.0 nM 7.31
CHEMBL2398258 — IC50 = 51.0 nM 7.29
CHEMBL2398253 — IC50 = 55.0 nM 7.26
CHEMBL2398261 — IC50 = 60.0 nM 7.22
CHEMBL2398263 — IC50 = 60.0 nM 7.22
CHEMBL2398259 — IC50 = 78.0 nM 7.11
CHEMBL2398256 — IC50 = 100.0 nM 7.00
CHEMBL2398286 — IC50 = 120.0 nM 6.92
CHEMBL2398172 — IC50 = 130.0 nM 6.89
CHEMBL2398289 — IC50 = 150.0 nM 6.82
CHEMBL2398251 — IC50 = 260.0 nM 6.58
CHEMBL2398262 — IC50 = 340.0 nM 6.47
CHEMBL2398283 — IC50 = 1100.0 nM 5.96
CHEMBL2398170 — IC50 = 1200.0 nM 5.92
CHEMBL2398285 — IC50 = 1300.0 nM 5.89
CHEMBL2398265 — IC50 = 1500.0 nM 5.82
CHEMBL2398284 — IC50 = 1500.0 nM 5.82
CHEMBL2398282 — IC50 = 1600.0 nM 5.80
CHEMBL2398171 — IC50 = 1700.0 nM 5.77
CHEMBL2398296 — IC50 = 1700.0 nM 5.77
CHEMBL2398266 — IC50 = 1800.0 nM 5.75
CHEMBL2398264 — IC50 = 2000.0 nM 5.70
CHEMBL2398292 — IC50 = 2200.0 nM 5.66
CHEMBL371861 — IC50 = 2200.0 nM 5.66
CHEMBL2398297 — IC50 = 2700.0 nM 5.57
CHEMBL2398288 — IC50 = 3800.0 nM 5.42
CHEMBL2398272 — IC50 = 4000.0 nM 5.40
CHEMBL2398277 — IC50 = 5200.0 nM 5.28
CHEMBL2398294 — IC50 = 6300.0 nM 5.20
CHEMBL2398267 — IC50 = 6700.0 nM 5.17
CHEMBL2398290 — IC50 = 7700.0 nM 5.11
CHEMBL2398287 — IC50 = 8100.0 nM 5.09
CHEMBL2398274 — IC50 = 9300.0 nM 5.03
CHEMBL2398291 — IC50 = 10000.0 nM 5.00
CHEMBL2398276 — IC50 = 15000.0 nM 4.82
CHEMBL2398273 — IC50 = 17000.0 nM 4.77
CHEMBL2398295 — IC50 = 76000.0 nM 4.12
CHEMBL2398293 — IC50 > 100000.0 nM -
CHEMBL2398298 — IC50 > 100000.0 nM -
CHEMBL2398268 — IC50 > 100000.0 nM -
CHEMBL2398269 — IC50 > 100000.0 nM -
CHEMBL2398270 — IC50 > 100000.0 nM -